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新型胃肠外给药青霉烯类药物舒洛培南对厌氧菌的体外抗菌活性

[In vitro activities of sulopenem, a new parenteral penem, against anaerobes].

作者信息

Watanabe K, Kato N, Tanaka-Bandoh K, Tanaka Y, Kato H, Ueno K

机构信息

Institute of Anaerobic Bacteriology, Gifu University School of Medicine.

出版信息

Jpn J Antibiot. 1996 Apr;49(4):367-76.

PMID:8786627
Abstract

In vitro activities of sulopenem, a novel parenteral penem, was compared with those of imipenem, flomoxef, cefuzonam, cefoperazone and sulbactam/ampicillin against 66 reference strains (19 genera, 61 species) and 392 recent clinical isolates of anaerobic bacteria and fastidious aerobic bacteria. Sulopenem had a very broad spectrum against anaerobic bacteria. In general, this compound was active against anaerobic reference strains with MICs of < or = 0.78 micrograms/ml, while being the least active against Bifidobacterium spp. and less active than imipenem against Lactobacillus spp. Sulopenem was more active against Bacteroides fragilis isolates than imipenem and had the highest activities against Bacteroides thetaiotaomicron, Prevotella intermedia, Porphyromonas gingivalis, Fusobacterium spp. and Peptostreptococcus spp. among the antibiotics tested. Sulopenem was not hydrolyzed by oxyiminocephalosporinase type 1 produced by B. fragilis GAI-0558, GAI-7955 and GAI-10150 and its stability was comparable to imipenem. Its susceptibilities to hydrolysis by a metallo-beta-lactamase from B. fragilis GAI-30144 was less than imipenem. Sulopenem (120 mg/kg, 3 times a day for 4 days) was as effective as imipenem/cilastatin against a mixed intraabdominal mice infection due to E. coli and B. fragilis. Sulopenem (20 mg/kg twice a day for 5 days) did not induce an overgrowth of Clostridium difficile in the caecum of mice.

摘要

将新型肠外青霉烯类药物舒巴坦尼的体外活性与亚胺培南、氟氧头孢、头孢唑南、头孢哌酮和舒巴坦/氨苄西林针对66株参考菌株(19个属,61个种)以及392株近期临床分离的厌氧菌和苛养需氧菌的活性进行了比较。舒巴坦尼对厌氧菌具有非常广泛的抗菌谱。总体而言,该化合物对MIC≤0.78微克/毫升的厌氧参考菌株具有活性,而对双歧杆菌属活性最低,对乳酸杆菌属的活性低于亚胺培南。舒巴坦尼对脆弱拟杆菌分离株的活性比亚胺培南更高,在测试的抗生素中,对多形拟杆菌、中间普雷沃菌、牙龈卟啉单胞菌、梭杆菌属和消化链球菌属的活性最高。舒巴坦尼不被脆弱拟杆菌GAI-0558、GAI-7955和GAI-10150产生的1型氧亚氨基头孢菌素酶水解,其稳定性与亚胺培南相当。它对脆弱拟杆菌GAI-30144产生的金属β-内酰胺酶的水解敏感性低于亚胺培南。舒巴坦尼(120毫克/千克,每日3次,共4天)在治疗由大肠杆菌和脆弱拟杆菌引起的小鼠腹腔混合感染方面与亚胺培南/西司他丁效果相当。舒巴坦尼(20毫克/千克,每日2次,共5天)未引起小鼠盲肠艰难梭菌过度生长。

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